PHARM: Antimalarials & Antianemia drugs Flashcards
Which antimalarial accumulates in the food vacuoles to inhibit the metabolism of heme?
Chloroquine!
Which plasmodium species have a dominant liver stage, and what drug could you give for it?
P. ovale and vivax!
Give PRIMAQUINE!
What can be a major side effect of Primaquine, and which patients are most at risk?
HEMOLYTIC ANEMIA
Patients with G6PD deficiency are most at risk
What can be a major side effect of quinines?
Cinchoism!
vertigo, blurred vision, nausea, etc
What does Rifampin do to P450?
INDUCES it!
So meds wear off faster
What are 3 main spp of plasmodium
P falciparum, vivax, and ovale
Which mosquito sp transmits malaria?
Anopheles
Plasmodium life cycle from sporozoite to merozoite
sporozoite in anopheles saliva, bites and sporos enter liver cells, multiply to form merozoites in liver cells (drug target), liver cells rupture and meros rel into blood where they invade RBCs, those lyse and it goes on to invade more RBCs
Plasmodium life cycle from RBC merozoites to asexuak and sexual life cycle
RBC merozoites feed on it (drug target), and can go on to enter asexual life cycle with 1 ring, 2 trophozoite, 3 schizont,
-but some differentiate into sexual parasites to produce gametes which mosquito can ingest now when it bites and transmit (drug target)
What produces the disease pathology in malaria?
RBCs rupture and release hemozoin, causing inflam
in falciparum, affects brain vasc causing seizure etc
Malaria treatment needs…
COMBINATION THERAPY!
What does chloroquine do?
accum in food vacuoles of parasite so it can’t digest heme
What does primaquine do? which form?
Treats LIVER form of p vivax/ovale
causes oxidative dmg on ETC
hemo anemia in G6PD-def patients
Which genes can confer resistance to Chloroquine?
pfcrt gene and PfMDR1, incr transporters to get drug out of food vacuole
What are 5 examples of drug combos for Chloroquine-resistant malaria?
1 Artimesinins (+lume) produce ROS
2 Atavaquone + Proguanil
3